GSK8612

Alias: GSK-8612; GSK 8612; GSK8612;
Cat No.:V4435 Purity: ≥98%
GSK8612 is a novel, potent and highly selective small molecule inhibitor ofTank-binding Kinase-1 (TBK1)with apIC50of 6.8 for recombinant TBK1.
GSK8612 Chemical Structure CAS No.: 2361659-62-1
Product category: TBK1
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

GSK8612 is a novel, potent and highly selective small molecule inhibitor of Tank-binding Kinase-1 (TBK1) with a pIC50 of 6.8 for recombinant TBK1. The serine/threonine protein kinase TBK1 (Tank-binding Kinase-1) is a noncanonical member of the IkB kinase (IKK) family. This kinase regulates signaling pathways in innate immunity, oncogenesis, energy homeostasis, autophagy, and neuroinflammation. In cellular assays, GSK861 inhibited toll-like receptor (TLR)3-induced interferon regulatory factor (IRF)3 phosphorylation in Ramos cells and type I interferon (IFN) secretion in primary human mononuclear cells. In THP1 cells, GSK8612 was able to inhibit secretion of interferon beta (IFNβ) in response to dsDNA and cGAMP, the natural ligand for STING. GSK8612 is a TBK1 small molecule inhibitor displaying an excellent selectivity profile and therefore represents an ideal probe to further dissect the biology of TBK1 in models of immunity, neuroinflammation, obesity, or cancer.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
GSK8612 suppresses type I IFN production in primary human mononuclear cells and toll-like receptor (TLR)3-induced IRF3 phosphorylation in Ramos cells. GSK8612 can prevent IFNβ from being secreted in THP1 cells in reaction to dsDNA and cGAMP, which is STING's natural ligand[1].
References
[1]. Thomson DW, et al. Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H17BRF3N7O2S
Molecular Weight
520.3268
CAS #
2361659-62-1
SMILES
O=S(C1=CC=C(CNC2=NC(NC3=CN(CC(F)(F)F)N=C3C)=NC=C2Br)C=C1)(N)=O
Chemical Name
4-((5-bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-ylamino)methyl)benzenesulfonamide
Synonyms
GSK-8612; GSK 8612; GSK8612;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 125 mg/mL (~240.23 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9219 mL 9.6093 mL 19.2186 mL
5 mM 0.3844 mL 1.9219 mL 3.8437 mL
10 mM 0.1922 mL 0.9609 mL 1.9219 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
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